Sparfosic acid trisodium | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Sparfosic acid trisodium 纯度: 99.65%

Sparfosic acid trisodium 是天门冬氨酸氨甲酰转移酶 (aspartate transcarbamoyl transferase) 的有效抑制剂，具有抗肿瘤和抗代谢物活性。天冬氨酸氨甲酰转移酶催化第二步 de novo 嘧啶生物合成。Sparfosic acid trisodium 协同增强 5-氟尿嘧啶 (5-FU) 和干扰素-α (IFN) 对人结肠癌细胞系的细胞毒性。

Sparfosic acid trisodium Chemical Structure

CAS No. : 70962-66-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4180	In-stock
5 mg	￥3800	In-stock
10 mg	￥6000	In-stock
50 mg	￥19800	In-stock
100 mg	￥29500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Sparfosic acid trisodium 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Anti-Cancer Compound Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library

生物活性

Sparfosic acid trisodium is a DNA antimetabolite agent and a potent inhibitor of aspartate transcarbamoyl transferase. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis. Sparfosic acid trisodium synergistically enhances the cytotoxicity of a combination of 5-fluorouracil (5-FU) and interferon-alpha (IFN) against human colon cancer cell lines^[1]^[2]^[3].

体外研究
(In Vitro)

Sparfosic acid (N-(Phosphonacetyl)-L-aspartate, PALA) treatment causes apoptosis in the resistant Br1 cells^[1].
Sparfosic acid (PALA, 300 µM) shows progressive accumulation of cells in S phase and activation of an apoptotic pathway leading to cell death^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

Cell Line:	Br-l and L-2 cell lines established from metastasis in nude mouse injected with the human tumor cell line MDA-MB-435.
Concentration:	300 µM.
Incubation Time:	12, 24 and 48 h.
Result:	Cells were predominantly in S phase in both the cell lines, although slightly higher proportion of cells in S phase were noted in L-2 than Brl-3prl cells.

Western Blot Analysis^[1]

Cell Line:	Br-l and L-2 cell lines.
Concentration:	300 µM.
Incubation Time:	4, 10 and 24 h.
Result:	There was moderate difference in the level of phosphorylated Rb proteins seen in the two cell types. Marked increase in the amount of cyclin A protein was detected in the L-2 cells undergoing apoptosis with the highest level detected at 10 h post-drug treatment. In contrast, there was no increase in the level of cyclin A seen in the Brl-3prl cells. Cyclin E protein was found elevated in the L-2 cells and Brl-3prl cells compared to their respective controls.

体内研究
(In Vivo)

Sparfosic acid (490 mg/kg; i.p.; on days 1, 5, and 9; mice bearing B16 melanoma) trisodium shows the life-span is increased survives 77 to 86% longer than controls. Lewis lung carcinoma is highly sensitive to Sparfosic acid trisodium. Treatment on days 1, 5, and 9 following s.c. implantation of Lewis lung carcinoma is curative to 50% of the mice^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

321.06

Formula

C₆H₇NNa₃O₈P

CAS 号

70962-66-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-80°C, protect from light, stored under nitrogen

溶解性数据

In Vitro:

H₂O : 250 mg/mL (778.67 mM; Need ultrasonic)

DMSO : 180 mg/mL (560.64 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1147 mL	15.5734 mL	31.1468 mL
5 mM	0.6229 mL	3.1147 mL	6.2294 mL
10 mM	0.3115 mL	1.5573 mL	3.1147 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

此方案可获得 ≥ 4.5 mg/mL (14.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

此方案可获得 ≥ 4.5 mg/mL (14.02 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 4.5 mg/mL (14.02 mM); Clear solution

此方案可获得 ≥ 4.5 mg/mL (14.02 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wang J, et al. Elevated cyclin A associated kinase activity promotes sensitivity of metastatic human cancer cells to DNA antimetabolite drug. Int J Oncol. 2015 Aug;47(2):782-90.

[2]. Angela D. Morris, et al. A New, Efficient, Two Step Procedure for the Preparation of the Antineoplastic Agent Sparfosic Acid

[3]. Wadler S, et al. Phase II trial of N-(phosphonacetyl)-L-aspartate (PALA), 5-fluorouracil and recombinant interferon-alpha-2b in patients with advanced gastric carcinoma. Eur J Cancer. 1996;32A(7):1254-1256.

[4]. Johnson RK, et al. Antitumor activity of N-(phosphonacetyl)-L-aspartic acid, a transition-state inhibitor of aspartate transcarbamylase. Cancer Res. 1976;36(8):2720-2725.

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